Gastrin and cholecystokinin receptor ligands (III)

Details Gastrin and cholecystokinin receptor ligands (III) Gastrin and cholecystokinin receptor ligands (III)

2006-04-25

2006-04-25

Shameem, Golam M. M. (Department: 1626)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C548S217000, C548S300100, C548S302700, C548S306100, C548S469000, C548S470000, C514S387000

Reexamination Certificate

active

07034048

ABSTRACT:
Compounds of formula (I) and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors. X and Y are independently ═N—, —N(R5)—(R5being selected from H, Me, Et, Pr, Bn, OH and —CH2COOR6, wherein R6represents H, Me, Et, Pr or Bn), ═CH—, —O— or —S—; n is from 1 to 4; A is an optionally substituted 5- or 6-membered carbocyclic ring wherein (a) 1 or 2 C atoms may optionally be replaced by N, O and/or S atoms, (b) A is fused with the aromatic group in formula (I) to form a fused bicycle, and (c) the ring containing X and Y is linked to a C atom of A; R1is H or C1to C15hydrocarbyl wherein up to three C atoms may optionally be replaced by N, O and/or S atoms and up to three H atoms may optionally be replaced by halogen atoms; R2is selected from H, Me, Et, Pr and OH, each R2being independently selected from H, Me, Et, Pr and OH when n is greater than 1; R3(when n is 1) is selected from H, Me, Et and Pr; or (when n is greater than 1) each R3is independently selected from H, Me, Et and Pr, or two R3groups on neighbouring carbon atoms are linked to form a C3to C6carbocylic ring, or two R3groups are absent from neighbouring carbon atoms which are linked by a double bond; or R2and R3on the same carbon atom together represent an ═O group; R4is C1to C15hydrocarbyl wherein up to two C atoms may optionally be replaced by N, O and/or S atoms and up to three H atoms may optionally be replaced by halogen atoms; V is —CO—NH—SO2—Ph, —SO2—NH—CO—PH, —CH2OH, or a group of the formula —R7U, (wherein U is —COOH, tetrazolyl, —CONHOH or —SO3H; and R7is a bond; C1to C6hydrocarbylene optionally substituted by hydroxy, amino or acetamido; —O—(C1to C3alkylene)—; —SO2NR8—CHR9—; —CO—NR8—CHR9—, R8and R9being independently selected from H and methyl; or —NH—(CO)c—CH2, c being 0 or 1); or a pharmaceutically acceptable salt thereof. Compositions comprising a compound a formula (I) are also described

REFERENCES:
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Susan E. Gibson et al., Incorporation of Conformationally Constrained Phenylalanine Derivatives TIC, SIC, HIC and NIC Into A Cholecystokinin-B/Gastrin Receptor Antagonist.
Patent Abstracts of Japan, JP 06 092961; Shikoku Chemical Corporation, Apr. 5, 1994.
E. Lindstrom et al., Pharmacological Analysis of CCK2 Receptor Antagonists Using Isolated Rat Stomach ECL Cells; British Journal of Pharmacology, vol. 127, 1999, pp. 530-536, XP001000286, p. 531, col. 1, paragraph 2.

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